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1 - Piperidinebutanamide, 4 - (4 - chlorophenyl) - 4 - hydroxy - N,N - dimethyl - alpha,alpha - diphenyl - , hydrochloride

RTECS #: TM4960000

CAS #: 34552-83-5

UPDATE: May 2009 MW: 513.55 MF: C29H33ClN2O2•ClH


NOTE:

TABLE OF CONTENTS:
  1. SYNONYMS:
  2. REPRODUCTIVE EFFECTS DATA:
  3. ACUTE TOXICITY DATA:
  4. OTHER MULTIPLE DOSE DATA:
  5. REVIEWS:
  6. NIOSH DOCUMENTATION AND SURVEILLANCE:
  7. REFERENCES:

SYNONYMS:

  1. 4 - (4 - (p - Chlorophenyl) - 4 - hydroxy - 1 - piperidyl) - N,N - dimethyl - 2,2 - diphenylbutyramide HCl
  2. 4 - (p - Chlorophenyl) - 4 - hydroxy - N,N - dimethyl - alpha,alpha - diphenyl - 1 - piperidine butyramide HCl
  3. BLOX
  4. BREK
  5. Dissenten
  6. Fortasec
  7. Imodium
  8. Imosec
  1. Lopemid
  2. Lopemin
  3. Loperamide hydrochloride
  4. Loperyl
  5. PJ185
  6. R 18553
  7. Suprasec
  8. Tebloc


SKIN AND EYE IRRITATION DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
N/R
 N/R N/R N/R


MUTATION DATA AND REFERENCES:

SYSTEM TEST ROUTE/
ORGANISM/
TISSUE 		DOSE REFERENCE
N/R N/R N/R N/R


REPRODUCTIVE EFFECTS DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
oral
rat 		lowest published toxic dose: 580 mg/kg (15-22 day pregnant/21 day after birth) Reproductive: Effects on newborn: Weaning or lactation index (e.g., # alive at weaning per # alive at day 4) ARZNAD 24,1645,1974


TUMORIGENIC DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
N/R
 N/R N/R N/R


ACUTE TOXICITY DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
intraperitoneal
mouse 		lethal dose (50 percent kill): 28 mg/kg Behavioral: Convulsions or effect on seizure threshold ARZNAD 24,1636,1974
intraperitoneal
mouse 		lowest published toxic dose: 0.63 mg/kg Nutritional and Gross Metabolic: Body temperature decrease JPETAB 302,1253,2002
intraperitoneal
mouse 		lowest published toxic dose: 2.5 mg/kg Behavioral: Somnolence (general depressed activity)

Nutritional and Gross Metabolic: Body temperature decrease 		PHTOEH 92,64,2003
intraperitoneal
rat 		lowest published toxic dose: 10 mg/kg Gastrointestinal: Decreased motility or constipation JPETAB 313,840,2005
intravenous
mouse 		lethal dose (50 percent kill): 12,640 µg/kg Behavioral: Tremor

Behavioral: Convulsions or effect on seizure threshold

Lung, Thorax, or Respiration: Other changes 		YACHDS 5,2419,1977
intravenous
rat 		lethal dose (50 percent kill): 7,490 µg/kg Behavioral: Somnolence (general depressed activity)

Behavioral: Muscle weakness

Lung, Thorax, or Respiration: Other changes 		YACHDS 5,2419,1977
oral
child 		lowest published toxic dose: 125 µg/kg Behavioral: Coma

Behavioral: Irritability

Cardiac: Pulse rate increased without fall in BP 		BMJOAE 294,1383,1987
oral
dog 		lowest published lethal dose: >40 mg/kg Gastrointestinal: Nausea or vomiting

Peripheral Nerve and Sensation: Flaccid paralysis without anesthesia (usually neuromuscular blockage) 		ARZNAD 24,1633,1974
oral
guinea pig 		lethal dose (50 percent kill): 41,500 µg/kg N/R IYKEDH 12,1204,1981
oral
monkey 		lethal dose (50 percent kill): >40 mg/kg Eye: Mydriasis (pupilliary dilation)

Gastrointestinal: Nausea or vomiting

Gastrointestinal: Decreased motility or constipation 		YACHDS 5,2419,1977
oral
mouse 		lethal dose (50 percent kill): 105 mg/kg N/R ARZNAD 24,1633,1974
oral
rat 		lethal dose (50 percent kill): 185 mg/kg Gastrointestinal: Decreased motility or constipation JMCMAR 16,782,1973
oral
rat 		lowest published toxic dose: 1 mg/kg Gastrointestinal: Decreased motility or constipation JPHSC* 104,263,2007
oral
rabbit 		lowest published lethal dose: 160 mg/kg Gastrointestinal: Decreased motility or constipation

Nutritional and Gross Metabolic: Body temperature decrease 		YACHDS 5,2419,1977
parenteral
rat 		lowest published toxic dose: 6 mg/kg Behavioral: Analgesia LIFSAK 71,2787,2002
subcutaneous
mouse 		lethal dose (50 percent kill): 75 mg/kg Behavioral: Convulsions or effect on seizure threshold ARZNAD 24,1636,1974
subcutaneous
mouse 		lowest published toxic dose: 0.3 mg/kg Gastrointestinal: Other changes JPETAB 314,1195,2005
subcutaneous
mouse 		lowest published toxic dose: 1 mg/kg Behavioral: Analgesia JPHSC* 104,218,2007
subcutaneous
rat 		lethal dose (50 percent kill): 78,700 µg/kg Eye: Mydriasis (pupilliary dilation)

Behavioral: Somnolence (general depressed activity)

Lung, Thorax, or Respiration: Other changes 		YACHDS 5,2419,1977
subcutaneous
rat 		lowest published toxic dose: 3 mg/kg Behavioral: Analgesia EJPHAZ 525,83,2005


OTHER MULTIPLE DOSE DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
oral
rat 		lowest published toxic dose: 900 mg/kg/30 day- intermittent Blood: Normocytic anemia

Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: Dehydrogenases

Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: Transaminases 		YACHDS 5,2419,1977
oral
rat 		lowest published toxic dose: 1,820 mg/kg/26 week- intermittent Cardiac: Changes in heart weight

Nutritional and Gross Metabolic: Changes in: Ca

Nutritional and Gross Metabolic: Weight loss or decreased weight gain 		YACHDS 5,2419,1977
subcutaneous
mouse 		lowest published toxic dose: 12 mg/kg/2 day- intermittent Behavioral: Analgesia JPHSC* 104,218,2007


REVIEWS:

ORGANIZATION STANDARD
REFERENCE
TOXICOLOGY REVIEW
HUTOX* -,473,1996


STANDARDS AND REGULATIONS:

ORGANIZATION STANDARD
REFERENCE
N/R N/R N/R


NIOSH DOCUMENTATION AND SURVEILLANCE:

ORGANIZATION STANDARD or SURVEY
REFERENCE
National Occupational Exposure Survey 1983 National Occupational Exposure Survey 1983: Hazard Code: X6146;
Number of Industries 1;
Total Number of Facilities 52;
Number of Occupations 2;
Total Number of Employees Exposed 1,035;
Total Number of Female Employees Exposed 563


STATUS IN FEDERAL AGENCIES:

ORGANIZATION
REFERENCE
N/R


REFERENCES:

CODEN
REFERENCE
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951-
BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857-
EJPHAZ European Journal of Pharmacology. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1967-
HUTOX*
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970-
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963-
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10-
JPHSC*
LIFSAK Life Sciences. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1-8, 1962-69; V.14- 1974-
PHTOEH Pharmacology and Toxicology (Copenhagen). (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.60- 1987-
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972-

Used as a long-acting antidiarrheal agent

FDA-proprietary drug

RTECS Compound Description:
   Drug
   Reproductive Effector
   Human Data

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